Preparation and antimicrobial assessment of 2-thioether-linked quinolonyl-carbapenems
| Autor: | Zoutendam Ph, Switzer Ag, T. P. Demuth, Tracy L. Twinem, Imbus R, Paula M. Koenigs, Paule Sm, Coleman Mc, Kraft Wg, Hershberger Pm, F. J. Rourke, Davis Bw, Devries Ca, Yelm Ke, Richard Siehnel |
|---|---|
| Rok vydání: | 1998 |
| Předmět: |
Penicillin binding proteins
medicine.drug_class Microbial Sensitivity Tests Muramoylpentapeptide Carboxypeptidase Quinolones Gram-Positive Bacteria Chemical synthesis chemistry.chemical_compound Structure-Activity Relationship Thioether Bacterial Proteins Multienzyme Complexes Drug Discovery Gram-Negative Bacteria medicine Penicillin-Binding Proteins Topoisomerase II Inhibitors Antibacterial agent Pharmacology Biological activity Quinolone Antimicrobial Biochemistry chemistry Carbapenems Hexosyltransferases Peptidyl Transferases Efflux Multidrug Resistance-Associated Proteins Carrier Proteins Cell Division |
| Zdroj: | The Journal of antibiotics. 51(9) |
| ISSN: | 0021-8820 |
| Popis: | This reports the synthesis and in vitro antimicrobial properties of a series of 2-thioether-linked quinolonyl-carbapenems. Although the title compounds exhibited broad spectrum activity, the MICs were generally higher than those observed for selected benchmark carbapenems, quinolonyl-penems, and quinolones. Enzyme assays suggested that the title compounds are potent inhibitors of penicillin binding proteins and inefficient inhibitors of bacterial DNA-gyrase. Uptake studies indicated that the new compounds are not substrates for the norA encoded quinolone efflux pump. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|